MDL | MFCD02585318 |
---|---|
Molecular Weight | 500.59 |
Molecular Formula | C21H28N2O8S2 |
SMILES | O=S(N1CCN(S(=O)(C2=CC=C(OC)C(OC)=C2)=O)CCC1)(C3=CC=C(OC)C(OC)=C3)=O |
SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.
TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
SB756050 is well‐tolerated; it is readily absorbed, exhibited nonlinear pharmacokinetics with a less than dose‐proportional increase in plasma exposure above 100 mg, and demonstrates no significant changes in exposure when co‐administered with sitagliptin. SB756050 demonstrates highly variable pharmacodynamic effects both within dose groups and between doses, with increases in glucose seen at the two lowest doses and no reduction in glucose seen at the two highest doses. The glucose effects of SB756050 sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT00733577 | GlaxoSmithKline |
Diabetes Mellitus, Type 2
|
August 11, 2008 | Phase 1 |
NCT00607906 | GlaxoSmithKline |
Diabetes Mellitus, Type 2
|
November 16, 2007 | Phase 1 |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : ≥ 150 mg/mL ( 299.65 mM )
* "≥" means soluble, but saturation unknown.
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.9976 mL | 9.9882 mL | 19.9764 mL |
5 mM | 0.3995 mL | 1.9976 mL | 3.9953 mL |
10 mM | 0.1998 mL | 0.9988 mL | 1.9976 mL |